Assay Detail
Binding
CHEMBL3119630
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincubated for 20 mins followed by glucose challenge measured after 40 mins by Hoechst 33342 staining-based assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | Hepatocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.10 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3114187 | — | — | 1 | 6.92 |
| CHEMBL3114185 | — | — | 1 | 6.70 |
| CHEMBL3114186 | — | — | 1 | 6.64 |
| CHEMBL3113985 | — | — | 1 | 6.62 |
| CHEMBL3114183 | — | — | 1 | 6.34 |
| CHEMBL3113980 | — | — | 1 | 6.09 |
| CHEMBL3113988 | — | — | 1 | 5.92 |
| CHEMBL3113987 | — | — | 1 | 5.89 |
| CHEMBL3113990 | — | — | 1 | 5.78 |
| CHEMBL3113986 | — | — | 1 | 5.77 |
| CHEMBL3113979 | — | — | 1 | 5.75 |
| CHEMBL3114188 | — | — | 1 | 5.53 |
| CHEMBL3113989 | — | — | 1 | 5.32 |
| CHEMBL3113999 | — | — | 1 | - |
| CHEMBL3113998 | — | — | 1 | - |
| CHEMBL3113997 | — | — | 1 | - |
| CHEMBL3113996 | — | — | 1 | - |
| CHEMBL3113995 | — | — | 1 | - |
| CHEMBL3113994 | — | — | 1 | - |
| CHEMBL3113993 | — | — | 1 | - |
| CHEMBL3113992 | — | — | 1 | - |
| CHEMBL3114190 | — | — | 1 | - |
| CHEMBL3113981 | — | — | 1 | - |
| CHEMBL3113982 | — | — | 1 | - |
| CHEMBL3113983 | — | — | 1 | - |
| CHEMBL3113984 | — | — | 1 | - |
| CHEMBL3113991 | — | — | 1 | - |
| CHEMBL3114000 | — | — | 1 | - |
| CHEMBL3114184 | — | — | 1 | - |
| CHEMBL3114189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3114187 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3114185 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3114186 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3113985 | — | EC50 | = | 239.0 | nM | 6.62 |
| CHEMBL3114183 | — | EC50 | = | 455.0 | nM | 6.34 |
| CHEMBL3113980 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3113988 | — | EC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL3113987 | — | EC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL3113990 | — | EC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL3113986 | — | EC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL3113979 | — | EC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL3114188 | — | EC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL3113989 | — | EC50 | = | 4760.0 | nM | 5.32 |
| CHEMBL3113999 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113998 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113997 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113996 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113995 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113994 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113993 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113992 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3114190 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113981 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113982 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113983 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113984 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3113991 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3114000 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3114184 | — | EC50 | > | 12500.0 | nM | - |
| CHEMBL3114189 | — | EC50 | > | 12500.0 | nM | - |